反应详情

温度

90 °C

Add 2-chloro-6-propanesulfonyl-isonicotinic acid methyl ester (2.70 g, 9.71 mmol), toluene (40 mL), palladium acetate (218 mg, 0.97 mmol), racemic 2,2′-bis(diphenylphosphino)-1,1′-binaphthyl (605 mg, 0.97 mmol), cesium carbonate (4.75 g, 14.6 mmol), and (S)-sec-butylamine (1.46 mL, 14.6 mmol) to a sealed vessel flushed with nitrogen. Heat and stir the sealed vessel at 90° C. overnight. Cool to room temperature, filter through a pad of filtering agent, concentrate and purify (silica gel chromatography, eluting with 20:80 to 30:70 ethyl acetate:hexanes) to give the title compound (2.47 g, 81%).

1. customflushed with nitrogen
2. temperatureHeat
3. temperatureCool to room temperature
4. filtrationfilter through a pad
5. filtrationof filtering agent
6. concentrationconcentrate
7. custompurify
8. wash(silica gel chromatography, eluting with 20:80 to 30:70 ethyl acetate:hexanes)